Lepirudin

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Lepirudin
Lepirudin sequence.svg
Systematic (IUPAC) name
[Leu1,Thr2]-63-desulfohirudin
Clinical data
Trade names Refludan
AHFS/Drugs.com monograph
Pregnancy cat.
Legal status
  • Prescription (US)
Routes SQ or IV
Pharmacokinetic data
Bioavailability 100
Half-life ~1.3 hours
Excretion Renal
Identifiers
CAS number 120993-53-5 YesY
ATC code B01AE02
DrugBank DB00001
UNII Y43GF64R34 N
KEGG D03692 YesY
ChEMBL CHEMBL1201666 N
Chemical data
Formula C288H448N80O110S6 
Mol. mass 6983.5 g/mol
 N (what is this?)  (verify)

Lepirudin is an anticoagulant that functions as a direct thrombin inhibitor.

Brand name: Refludan, Generic: Lepirudin rDNA for injection.

Lepirudin is a recombinant hirudin[1] derived from yeast cells. It is almost identical to hirudin extracted from Hirudo medicinalis. It differs by the substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63.

Lepirudin may be used as an anticoagulant when heparins (unfractionated or low-molecular-weight) are contraindicated because of heparin-induced thrombocytopenia.

Market Withdrawal[edit]

Bayer has announced that it will cease the production of lepirudin (Refludan) effective May 31, 2012.[2]

References[edit]

  1. ^ Arman T. Askari; A. Michael Lincoff (October 2009). Antithrombotic Drug Therapy in Cardiovascular Disease. Springer. pp. 440–. ISBN 978-1-60327-234-6. Retrieved 30 October 2010. 
  2. ^ http://www.fda.gov/drugs/drugsafety/drugshortages/ucm050794.htm

External links[edit]

  • DDB 30082
  • Smythe M, Stephens J, Koerber J, Mattson J (2005). "A comparison of lepirudin and argatroban outcomes.". Clin Appl Thromb Hemost 11 (4): 371–4. doi:10.1177/107602960501100403. PMID 16244762. 
  • Tardy, B; Lecompte, T; Boelhen, F; Tardy-Poncet, B; Elalamy, I; Morange, P; Gruel, Y; Wolf, M; François, D (2006). "Predictive factors for thrombosis and major bleeding in an observational study in 181 patients with heparin-induced thrombocytopenia treated with lepirudin". Blood 108 (5): 1492–6. doi:10.1182/blood-2006-02-001057. PMID 16690967. 
  • Lubenow N, Eichler P, Lietz T, Greinacher A (2005). "Lepirudin in patients with heparin-induced thrombocytopenia - results of the third prospective study (HAT-3) and a combined analysis of HAT-1, HAT-2, and HAT-3.". J Thromb Haemost 3 (11): 2428–36. doi:10.1111/j.1538-7836.2005.01623.x. PMID 16241940.